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作者建立了测定法莫替丁血药浓度的高效液相色谱方法,并对正常志愿者静脉注射法莫替丁的药物动力学和药效学进行了研究。结果表明,药物动力学符合开放性二室模型,终端消除半减期3.16h;表观分布容积99.40L;总体清除率392.12ml/min;药时曲线下面积1057.45h ng/ml;胃液pH值、分泌量和胃酸分泌量等药效学指标测定表明,单剂量静脉注射法莫替丁20mg,体内有效作用时间可持续8～9h。以Hill作图法描述了血药浓度与药效学(胃酸抑制率)的关系,推导出描述血药浓度与药效的数学关系式为E=100·C~(2.60)/(C~(2.60)+14.71~(2.60)),用此数学模型可由血药浓度预测药效,或由药效预测血药浓度。
The authors established a high performance liquid chromatography method for the determination of famotidine plasma concentration, and studied the pharmacokinetics and pharmacodynamics of intravenous famotidine in normal volunteers. The results showed that the pharmacokinetics conformed to the open two-compartment model, terminal elimination half-time 3.16h; apparent volume of distribution 99.40L; total clearance rate 392.12ml / min; the area under the curve of drug time 1057.45h ng / ml; , Secretion and gastric acid secretion and other pharmacodynamic indicators measured showed that single-dose intravenous injection of famotidine 20mg, effective duration of the body can be sustained 8 ~ 9h. The relationship between plasma concentration and pharmacodynamics (gastric acid inhibition rate) was described by Hill mapping. The mathematical relationship between plasma concentration and pharmacodynamics was deduced as E = 100 · C ~ (2.60) / (C ~ 2.60) +14.71 ~ (2.60)). Using this mathematical model, the drug efficacy can be predicted from the plasma concentration or the plasma concentration can be predicted from the pharmacodynamic effect.